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Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model.
(American Society for Pharmacology and Experimental Therapeutics, 2003-08-01)
Knowing the importance for research and pharmacological uses of proper ligand classification into agonists, inverse agonists, and antagonists, the aim of this work was to study the behavior of tiotidine, a controversial ...
Rapid desensitization and slow recovery of the cyclic AMP response mediated by histamine H2 receptors in the U937 cell line
(Pergamon-Elsevier Science Ltd., 2000-07-15)
The present study focused on the desensitization process of the H(2) receptor in U937 cells and the recovery of the cyclic AMP (cAMP) response. Treatment of U937 leukemic cells with the H(2) histamine receptor agonists ...
Signal transduction mechanism of biased ligands at histamine H2 receptors
(Portland Press, 2014-04-01)
7TMRs (seven-transmembrane receptors) exist as conformational collections in which different conformations would lead to differential downstream behaviours such as receptor phosphorylation, G-protein activation and receptor ...